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United States Patent | 6,180,642 |
Walsh ,   et al. | January 30, 2001 |
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
Inventors: | Walsh; Thomas F. (Watchung, NJ); Ujjainwalla; Feroze (Edison, NJ) |
Assignee: | Merck & Co., Inc. (Rahway, NJ) |
Appl. No.: | 520318 |
Filed: | March 7, 2000 |
Current U.S. Class: | 514/299; 514/300; 546/112; 546/113 |
Intern'l Class: | A61K 031/495; C07D 221/02; C07D 471/02 |
Field of Search: | 546/113,112 514/300,299 |
4544663 | Oct., 1985 | Manning et al. | |
5030640 | Jul., 1991 | Fisher et al. | |
5756507 | May., 1998 | Goulet et al. | |
5780437 | Jul., 1998 | Goulet et al. | |
5849764 | Dec., 1998 | Goulet et al. | |
Foreign Patent Documents | |||
879 381 | Feb., 1980 | BE. | |
679 642 | Nov., 1995 | EP. | |
2 181 559 | Dec., 1973 | FR. | |
WO 90/05721 | May., 1990 | WO. | |
WO 95/29900 | Nov., 1995 | WO. | |
WO 97/21707 | Jun., 1997 | WO. | |
WO 97/21703 | Jun., 1997 | WO. |
Annu. Rev. Med., vol. 45, pp. 391-405 (1994), by Conn, et al. Drugs of the Future, vol. 13, No. 8. pp. 761-787 (1988), by A. S. Dutta. Current Opinion in Obstetrics & Gynocology, vol. 6, pp. 262-268 (1994), by R. A. Loy. TEM, vol. 3, No. 1, pp. 30-34 (1992), by R. L. Barbieri. Drugs, vol. 35, pp. 63-82 (1988), by Filicori, et al. Human Reproduction, vol. 11, Suppl. 1 (1996), by G. Hodgen. Human Reproduction, vol. 11, Suppl. 3 (1996), by U. Cirkel. J. of the Chemical Society, pp. 459-463 (1970), by Herbert, et al. J. Med. Chem., vol. 32, pp. 2036-2038 (1989), by Clark, et al. |
##STR19## Ex. X--R.sub.7, R.sub.8 --(A)--R.sub.1 3A ##STR20## ##STR21## 3B ##STR22## ##STR23## 3C ##STR24## ##STR25## 3D ##STR26## ##STR27##